87223-76-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 2-alkoxycarbonyl-3-anilinoindoles as a new class of potent inhibitors of tubulin polymerization
Balzarini, Jan,Bortolozzi, Roberta,Brancale, Andrea,Ferla, Salvatore,Hamel, Ernest,Kimatrai Salvador, Maria,Liekens, Sandra,Oliva, Paola,Persoons, Leentje,Prencipe, Filippo,Romagnoli, Romeo,Schols, Dominique,Viola, Giampietro
, (2020/02/22)
A new class of inhibitors of tubulin polymerization based on the 2-alkoxycarbonyl-3-(3′,4′,5′-trimethoxyanilino)indole molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization and cell cycle eff
Identification of substituted pyrimido[5,4-b]indoles as selective toll-like receptor 4 ligands
Chan, Michael,Hayashi, Tomoko,Mathewson, Richard D.,Nour, Afshin,Hayashi, Yuki,Yao, Shiyin,Tawatao, Rommel I.,Crain, Brian,Tsigelny, Igor F.,Kouznetsova, Valentina L.,Messer, Karen,Pu, Minya,Corr, Maripat,Carson, Dennis A.,Cottam, Howard B.
, p. 4206 - 4223 (2013/07/19)
A cell-based high-throughput screen to identify small molecular weight stimulators of the innate immune system revealed substituted pyrimido[5,4-b]indoles as potent NFκB activators. The most potent hit compound selectively stimulated Toll-like receptor 4 (TLR4) in human and mouse cells. Synthetic modifications of the pyrimido[5,4-b]indole scaffold at the carboxamide, N-3, and N-5 positions revealed differential TLR4 dependent production of NFκB and type I interferon associated cytokines, IL-6 and interferon γ-induced protein 10 (IP-10) respectively. Specifically, a subset of compounds bearing phenyl and substituted phenyl carboxamides induced lower IL-6 release while maintaining higher IP-10 production, skewing toward the type I interferon pathway. Substitution at N-5 with short alkyl substituents reduced the cytotoxicity of the leading hit compound. Computational studies supported that active compounds appeared to bind primarily to MD-2 in the TLR4/MD-2 complex. These small molecules, which stimulate innate immune cells with minimal toxicity, could potentially be used as adjuvants or immune modulators.
Interleukin-4 gene expression inhibitors
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, (2008/06/13)
This invention discloses and claims a class of indole and benzo(b)thiophene derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. The compounds of this invention are defined by the Formula (I): wherein X, Y, Z, R1, R2 and R3 are as defined in the specification; or a pharmaceutically acceptable salt thereof. In preferred embodiments of this invention it is also disclosed and claimed that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
CERTAIN ARYL FUSED PYRROLOPYRIMIDINES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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, (2008/06/13)
The present invention encompasses structures of the formula: STR1 and the pharmaceutically acceptable non-toxic salts thereof wherein: STR2 and X represents hydrogen, halogen, or hydroxy; W represents an aryl group unsubstituted or substituted with
Pyridopyrimidoindoles. A New Heterocyclic Ring System
Unangst, Paul C.
, p. 495 - 499 (2007/10/02)
The preparation of the novel pyridopyrimidoindole ring system is described via fusion at 180 deg C of ethyl 3-amino-1H-indole-2-carboxylate 8a and several 6-chloronicotinic acid derivatives.Similar fusion of 8a and thiourea yielded a 2-m
